Enzymes as Targets for Drug Design is a collection of scientific discussions related to enzyme inhibitors that show the many facets of the drug discovery process from the basic sciences through clinical applications. Topics include the biogenesis of phosphatidylinositol glycosyl membrane proteins, structure and catalytic function of ADP-ribose polymerase (ADPRT), and modulation of the dopaminergic system in cardiovascular therapeutics. The therapeutic utility of selected enzyme-activated irreversible inhibitors, the role of proteinases in the fibrosis of systemic sclerosis, and therapeutic opportunities in eicosanoid biosynthesis are also discussed. This book consists of 18 chapters and begins with examples of enzymes whose activities have recently been elucidated, or for which newer insights have been gleaned, but which do not yet have selective or potent inhibitors. The second part provides examples of enzymes where inhibitors have been identified but it is still not clear whether or not such an enzymatic blockade will be therapeutically beneficial. The final section describes clinical studies of newer, and not so new, enzyme inhibitors that are clearly of therapeutic importance. The therapeutic activity of monoamine oxidase inhibitors and the associated clinical issues are considered. This book is intended for clinicians as well as basic scientists in biochemistry, chemistry, pharmacology, and cell biology.
7.3.2 Limits on K?” Determinations Use of Morrison's quadratic equation, together with Murphy's recommended dilution scheme, will allow accurate estimates of K f'pp as low as 100-fold below the total enzyme concentration.
This book provides vital information on a class of enzymes that have emerged as key drug targets in a number of human diseases, including HIV/AIDS, Hypertension, Cancer, and Alzheimer's disease.
Drug Design of Zinc-Enzyme Inhibitors brings together functional and structural information relevant to these zinc-containing targets.
This book helps medicinal chemists and pharmacologists to do exactly that in the realm of enzyme inhibitors.
Sets the stage for advances in drug discovery using the latest enzyme technology Reviewing new and emerging applications of enzyme technology in drug discovery, this book highlights some of the most promising areas of pharmaceutical and ...
The book discusses: The drug discovery process, including drug discovery strategy, medicinal chemistry, analytical chemistry, drug metabolism, pharmacokinetics, and safety biomarker assessment The manipulations of drug metabolizing enzymes ...
The book focuses on enzyme mechanisms, and introduces key drugs that target each type and subtype of enzyme, and describes, with figures and arrow-pushing diagrams, how these inhibitors work.
This is a valuable reference for academic and industrial researchers in medicinal chemistry, drug design and development, pharmacology, biochemistry, and molecular and cell biology.
This book offers deep insights into the thermodynamics and molecular structures of the twelve catalytically active isoforms of human carbonic anhydrase (CA) with a particular focus on inhibitor binding for drug design.
Readers will applaud this book for its clear and practical presentations, including its expert advice on best practices to follow and pitfalls to avoid.